کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1372967 981886 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: Part 1
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: Part 1
چکیده انگلیسی

The observation that 17-cyclopropylmethylmorphinan derivatives without the 4,5-epoxy ring showed more κ selectivity than those with a 4,5-epoxy ring led us to develop a working hypothesis: the position of the plane composed of the A and B rings would influence the opioid receptor type selectivity and that the decrease in the torsion angle C11–C12–C13–C14 could improve the κ selectivity. Consistent with our hypothesis, KNT-42 with an N-cyclopropylmethyl propellane structure, whose A and B rings were fixed in a torsion angle of approximately 0°, showed κ selective agonist activity.

Propellane derivative KNT-42 showed rather κ selective agonist activity.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 13, 1 July 2011, Pages 4104–4107
نویسندگان
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